合成具有组氨酸样螯合作用的卟啉：分子 PDT/SPECT 治疗的有效途径。
Synthesis of a porphyrin with histidine-like chelate: an efficient path towards molecular PDT/SPECT theranostics.
机构信息
Department of Chemistry and Biochemistry, Faculty of Science and Engineering, University of Hull, HU6 7RX, UK.
Department of Biomedical Sciences, University of Hull, Cottingham Road, Hull, HU6 7RX, UK and Positron Emission Tomography Research Centre, University of Hull, Cottingham Road, Hull, HU6 7RX, UK.
出版信息
Chem Commun (Camb). 2020 Sep 22;56(75):11090-11093. doi: 10.1039/d0cc03958f.
The goal of "personalised" medicine has seen a growing interest in the development of theranostic agents. Bifunctional, and targeted-trifunctional, theranostic water-soluble porphyrins with a histidine-like chelating group have been synthesised via copper-catalysed azide-alkyne cycloaddition (CuAAC) "click" chemistry in high yield and purity. They are capable of photodynamic treatment and [99mTc(CO)3]+ complexation for single-photon emission computed tomography (SPECT) imaging, with a radiochemical yield of >95%. The toxicity and phototoxicity were evaluated on HT-29 cells, DU145, and DU145-PSMA cell lines, with the targeted theranostic showing more potent phototoxicity towards DU145-PSMA expressing cells.
“个性化”医学的目标促使人们对治疗诊断试剂的发展产生了浓厚的兴趣。通过铜催化的叠氮-炔环加成（CuAAC）“点击”化学，合成了具有组氨酸样螯合基团的双功能和靶向三功能治疗诊断水溶性卟啉，产率和纯度都很高。它们能够进行光动力治疗，并与[99mTc（CO）3]+配合进行单光子发射计算机断层扫描（SPECT）成像，放射化学产率>95%。在 HT-29 细胞、DU145 和 DU145-PSMA 细胞系上评估了其毒性和光毒性，靶向治疗诊断试剂对表达 PSMA 的 DU145-PSMA 细胞表现出更强的光毒性。
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